Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases

  • Eur J Med Chem. 2007 Feb;42(2):243-7. doi: 10.1016/j.ejmech.2006.09.014.
Laurent Brault  1 ,  Mickaël Denancé ,  Estelle Banaszak ,  Souhayla El Maadidi ,  Eric Battaglia ,  Denyse Bagrel ,  Mohammad Samadi
Affiliations
  • 1. LIMBP, Université Paul Verlaine-Metz, Metz Technopôle, 57078 Metz, France.
PMID: 17084000 DOI: 10.1016/j.ejmech.2006.09.014
Abstract

An efficient synthesis of dialkylsubstituted maleic anhydrides 1a-j is described. The inhibitory potential of these original anhydride derivatives was tested toward the three human isoforms A, B and C of dual specific phosphatases Cdc25. A micromolar range inhibition of Cdc25s was observed with the maleic anhydrides bearing simple alkyl side chains longer than C(9), to reach the optimal activity with a C(17) chain length.

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